Direct C-2 Arylation of 7-Azaindoles: Chemoselective Access to Multiarylated Derivatives

Pd-catalyzed direct C-H arylation of N-methyl-7-azaindole at the C-2 position by diverse arylboronic acids was achieved at room temperature. The method is general and was applied in chemoselective synthesis of multiarylated 7-azaindole derivatives bearing three different aryl groups at the 2, 3, and 5 positions.